Nicotinamide-based Compounds as Potent Inhibitors of Translational- and Transcriptional-related Kinases
Tumor-tropic S. Typhimurium strain that reprograms immune microenvironments to destroy cold solid tumors.
Researchers at Purdue University have designed molecules to concurrently inhibit two proteins important in tumorigenesis, MNK1/2 and p70S6K. Pharmaceutical companies have pursued MNK1/2 and p70S6K as individual targets; however, drugs targeting these proteins performed poorly as monotherapies. By inhibiting both MNK1/2 and p70S6K with a single molecule, the Purdue researchers' orally bioavailable compounds potently inhibit several solid tumor cancer cell lines, including breast, ovarian, lung, and colon cancer cells.
Technology Validation: At 200 nM, one of the drugs designed by the researchers completely inhibited the growth of Caki-1 (renal cancer) and MDA-MB-231 (breast cancer) cells. Compounds were tested against the NCI-60 cell line panel.
Advantages
- Targets two oncogenic proteins with a single molecule
- Effective against multiple solid tumor cell lines
- Orally bioavailable
Applications
- Anticancer drugs
Publication:
https://www.sciencedirect.com/science/article/pii/S0045206825001786
TRL: Pharmaceuticals
Intellectual Property:
Provisional-Patent, 2022-04-06, United States
PCT-Patent, 2023-04-06, WO
NATL-Patent, 2023-04-06, Europe
NATL-Patent, 2023-04-06, Japan
NATL-Patent, 2023-04-06, China
NATL-Patent, 2023-04-06, Canada
NATL-Patent, 2024-10-04, United States
Keywords: Cancer, Kinase inhibitor, MNK, Oncology, p70S6K, Pharmaceuticals, Solid Tumor